| Literature DB >> 23265892 |
Wen-Lian Wu1, Theodros Asberom, Thomas Bara, Chad Bennett, Duane A Burnett, John Clader, Martin Domalski, William J Greenlee, Hubert Josien, Mark McBriar, Murali Rajagopalan, Monica Vicarel, Ruo Xu, Lynn A Hyde, Robert A Del Vecchio, Mary E Cohen-Williams, Lixin Song, Julie Lee, Giuseppe Terracina, Qi Zhang, Amin Nomeir, Eric M Parker, Lili Zhang.
Abstract
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease. Specifically, 4-CF(3) and 4-Br substituted arylsulfone analogs, (-)-1b and (-)-1c, are equipotent to compound (-)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated.Entities:
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Year: 2012 PMID： 23265892 DOI： 10.1016/j.bmcl.2012.11.047
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823